Stopping Relapse Behaviors in Individuals Addicted to Cocaine

Posted on May 14, 2014 at 12:49 pm

A University of Buffalo animal study has found a compound that targets an important brain receptor that has a significant effect against cocaine addiction behaviors—including relapse behaviors.[1] Therefore, the research has provided the scientific community with evidence that may lead to new treatments for cocaine addiction, as currently no effective medications exist.1 The compound, RO5263397, was found to blunt a wide range of cocaine addiction behaviors.1

“This is the first systematic study to convincingly show that RO5263397 has the potential to treat cocaine addiction,” said Jun-Xu Li, MD, PhD, senior author of the study. “Our research shows that trace amine associated receptor 1—TAAR 1—holds great promise as a novel drug target for the development of novel medications for cocaine addiction.”1

TAAR 1 is a receptor in the brain that is activated by small amounts of brain chemicals called trace amines.1 The compound targets TAAR 1, which is expressed in key drug reward and addiction regions of the brain.1

“Because TAAR 1 anatomically and neurochemically is closely related to dopamine—one of the key molecules in the brain that contributes to cocaine addiction—and is thought to be a “brake” on dopamine activity, drugs that stimulate TAAR 1 may be able to counteract cocaine addiction,” said Li.1

University of Buffalo researchers tested their hypothesis by using a newly developed TAAR 1 agonist RO5263397, a drug that stimulates TAAR 1 receptors, in animal models.1 They used the conditioned place preference, where the animal’s persistence in returning to, or staying at, the physical location where the drug was given, is interpreted to indicate the drug’s rewarding effects.1 They found that RO5263397 significantly blocked cocaine’s rewarding effects.1

“When we give the rats RO5263397, they no longer perceive cocaine rewarding, suggesting that the primary effect that drives cocaine addiction in humans has been blunted,” said Li. “Cocaine users often stay clean for some time, but may relapse when they re-experience cocaine or hang out in the old cocaine use environments. We found that RO5263397 markedly blocked the effect of cocaine or cocaine-related cues for priming relapse behavior.”1

Li added, “Also, when we measured how hard the animals are willing to work to get an injection of cocaine, RO5263397 reduced the animals’ motivation to get cocaine. This compound makes rats less willing to work for cocaine, which led to decreased cocaine use.”1